CA2575340A1 - Macrocyclic beta-secretase inhibitors - Google Patents

Macrocyclic beta-secretase inhibitors Download PDF

Info

Publication number
CA2575340A1
CA2575340A1 CA002575340A CA2575340A CA2575340A1 CA 2575340 A1 CA2575340 A1 CA 2575340A1 CA 002575340 A CA002575340 A CA 002575340A CA 2575340 A CA2575340 A CA 2575340A CA 2575340 A1 CA2575340 A1 CA 2575340A1
Authority
CA
Canada
Prior art keywords
compound
alkyl
effective amount
group
mmol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA002575340A
Other languages
English (en)
French (fr)
Inventor
Andrew W. Stamford
Ying Huang
Guoqing Li
Corey O. Strickland
Johannes H. Voigt
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme Corp
Original Assignee
Schering Corporation
Andrew W. Stamford
Ying Huang
Guoqing Li
Corey O. Strickland
Johannes H. Voigt
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corporation, Andrew W. Stamford, Ying Huang, Guoqing Li, Corey O. Strickland, Johannes H. Voigt filed Critical Schering Corporation
Publication of CA2575340A1 publication Critical patent/CA2575340A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA002575340A 2004-07-28 2005-07-26 Macrocyclic beta-secretase inhibitors Abandoned CA2575340A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US59189904P 2004-07-28 2004-07-28
US60/591,899 2004-07-28
PCT/US2005/026468 WO2006014944A1 (en) 2004-07-28 2005-07-26 Macrocyclic beta-secretase inhibitors

Publications (1)

Publication Number Publication Date
CA2575340A1 true CA2575340A1 (en) 2006-02-09

Family

ID=35106859

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002575340A Abandoned CA2575340A1 (en) 2004-07-28 2005-07-26 Macrocyclic beta-secretase inhibitors

Country Status (13)

Country Link
US (2) US7652003B2 (xx)
EP (1) EP1781644B1 (xx)
JP (1) JP2008508289A (xx)
CN (1) CN101027297B (xx)
AR (1) AR050184A1 (xx)
AT (1) ATE396990T1 (xx)
CA (1) CA2575340A1 (xx)
DE (1) DE602005007245D1 (xx)
ES (1) ES2306200T3 (xx)
HK (1) HK1102328A1 (xx)
MX (1) MX2007001102A (xx)
TW (1) TWI297337B (xx)
WO (1) WO2006014944A1 (xx)

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US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
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CA2610812A1 (en) * 2005-06-14 2006-12-28 Schering Corporation Aspartyl protease inhibitors
PL1976877T5 (pl) 2005-11-30 2017-09-29 Abbvie Inc Przeciwciała monoklonalne przeciwko białku amyloidu beta oraz ich zastosowania
CN117903302A (zh) 2005-11-30 2024-04-19 Abbvie 公司 抗-Aβ球聚体抗体,其相关产品,生产所述抗体的方法,所述抗体的应用以及使用方法
EP2032542A2 (en) 2006-06-12 2009-03-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
AU2007275132A1 (en) * 2006-07-20 2008-01-24 Novartis Ag Macrocyclic lactams
AU2007307170A1 (en) 2006-10-06 2008-04-17 Merck & Co., Inc. Macrocyclic spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease
WO2008055945A1 (en) 2006-11-09 2008-05-15 Probiodrug Ag 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
US8455626B2 (en) 2006-11-30 2013-06-04 Abbott Laboratories Aβ conformer selective anti-aβ globulomer monoclonal antibodies
EP2091948B1 (en) 2006-11-30 2012-04-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
KR20090087487A (ko) 2006-12-12 2009-08-17 쉐링 코포레이션 아스파르틸 프로테아제 억제제
EP2486928A1 (en) 2007-02-27 2012-08-15 Abbott GmbH & Co. KG Method for the treatment of amyloidoses
MX2009009234A (es) 2007-03-01 2009-12-01 Probiodrug Ag Uso nuevo de inhibidores de ciclasa de glutaminilo.
EP2865670B1 (en) 2007-04-18 2017-01-11 Probiodrug AG Thiourea derivatives as glutaminyl cyclase inhibitors
US8518975B2 (en) 2007-09-06 2013-08-27 Merck Sharp + Dohme Corp. Gamma secretase modulators
EP2217604A1 (en) 2007-11-05 2010-08-18 Schering Corporation Gamma secretase modulators
WO2009076352A1 (en) * 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
TW200948364A (en) 2008-04-22 2009-12-01 Schering Corp Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
CA2742486A1 (en) 2008-11-13 2010-05-20 Schering Corporation Gamma secretase modulators
AU2009330233A1 (en) 2008-12-22 2011-07-07 Merck Sharp & Dohme Corp. Gamma secretase modulators
CA2747750A1 (en) 2008-12-22 2010-07-01 Theodros Asberom Gamma secretase modulators
EP2443121A2 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
US20120245158A1 (en) 2009-06-16 2012-09-27 Xianhai Huang Gamma secretase modulators
US20120232108A1 (en) 2009-06-16 2012-09-13 Xianhai Huang Gamma secretase modulators
ES2548913T3 (es) 2009-09-11 2015-10-21 Probiodrug Ag Derivados heterocíclicos como inhibidores de glutaminil ciclasa
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
US8563543B2 (en) 2009-10-08 2013-10-22 Merck Sharp & Dohme Corp. Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US8557826B2 (en) 2009-10-08 2013-10-15 Merck Sharp & Dohme Corp. Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
AU2011226074B2 (en) 2010-03-10 2015-01-22 Vivoryon Therapeutics N.V. Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
CA2796339C (en) 2010-04-15 2020-03-31 Abbott Laboratories Amyloid-beta binding proteins
EP2560953B1 (en) 2010-04-21 2016-01-06 Probiodrug AG Inhibitors of glutaminyl cyclase
CA2808187A1 (en) 2010-08-14 2012-02-23 Abbvie Inc. Amyloid-beta binding proteins
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
WO2012138734A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. C5-c6 oxacyclic-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
EP2747769B1 (en) 2011-08-22 2017-08-02 Merck Sharp & Dohme Corp. 2-spiro-substituted iminothiazines and their mono-and dioxides as bace inhibitors, compositions and their use
WO2013142370A1 (en) 2012-03-19 2013-09-26 Varghese John APP SPECIFIC BACE INHIBITORS (ASBIs) AND USES THEREOF
WO2014056816A1 (en) 2012-10-10 2014-04-17 F. Hoffmann-La Roche Ag COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR
WO2014062549A1 (en) 2012-10-17 2014-04-24 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US9416129B2 (en) 2012-10-17 2016-08-16 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US10202355B2 (en) 2013-02-12 2019-02-12 Buck Institute For Research On Aging Hydantoins that modulate bace-mediated app processing
CN105175488A (zh) * 2015-09-07 2015-12-23 西北农林科技大学 一种具有抗老年痴呆症活性的化合物及其制备方法
DK3461819T3 (da) 2017-09-29 2020-08-10 Probiodrug Ag Inhibitorer af glutaminylcyklase

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EP0395664A1 (en) 1987-10-21 1990-11-07 The Upjohn Company Renin inhibitors containing a (1-amino-2-hydroxy-2-heterocyclic) ethyl moiety
PE20020276A1 (es) 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
ES2248356T3 (es) 2000-06-30 2006-03-16 Elan Pharmaceuticals, Inc. Compuestos para tratar la enfermedad de alzheimer.
US6846813B2 (en) 2000-06-30 2005-01-25 Pharmacia & Upjohn Company Compounds to treat alzheimer's disease
US20030095958A1 (en) 2001-04-27 2003-05-22 Bhisetti Govinda R. Inhibitors of bace
JP2005505506A (ja) * 2001-06-12 2005-02-24 イーラン ファーマスーティカルズ、インコーポレイテッド アルツハイマー病の治療に有用な大環状分子
DE60210614T2 (de) 2001-06-12 2007-03-01 Elan Pharmaceuticals, Inc., South San Francisco Für die behandlung von alzheimerkrankheit geeignete makrocyclen
US20040171614A1 (en) 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
ATE443043T1 (de) * 2002-11-12 2009-10-15 Merck & Co Inc Phenylcarboxamide als beta-sekretase-hemmer zur behandlung von alzheimer
AU2004204692B2 (en) * 2003-01-07 2009-07-09 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of Alzheimer's disease
AU2005264917A1 (en) 2004-06-16 2006-01-26 Wyeth Diphenylimidazopyrimidine and -imidazole amines as inhibitors of B-secretase
PE20060459A1 (es) 2004-06-16 2006-05-30 Wyeth Corp DERIVADOS DE AMINO-5,5-DIFENILIMIDAZOLONA COMO INHIBIDORES DE LA ß-SECRETASA
WO2007005404A1 (en) 2005-06-30 2007-01-11 Wyeth AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION
TW200738683A (en) 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
TW200730523A (en) 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
EP2256107A1 (en) 2005-09-26 2010-12-01 Wyeth LLC Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds as inhibitors of the beta-secretase (BACE)
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TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
TW200815449A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200808796A (en) 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
TW200815349A (en) 2006-06-22 2008-04-01 Astrazeneca Ab New compounds

Also Published As

Publication number Publication date
DE602005007245D1 (xx) 2008-07-10
US8012953B2 (en) 2011-09-06
ES2306200T3 (es) 2008-11-01
MX2007001102A (es) 2007-04-13
ATE396990T1 (de) 2008-06-15
EP1781644A1 (en) 2007-05-09
JP2008508289A (ja) 2008-03-21
US20100178294A1 (en) 2010-07-15
AR050184A1 (es) 2006-10-04
EP1781644B1 (en) 2008-05-28
CN101027297B (zh) 2010-09-08
HK1102328A1 (en) 2007-11-16
TW200607807A (en) 2006-03-01
TWI297337B (en) 2008-06-01
WO2006014944A1 (en) 2006-02-09
US7652003B2 (en) 2010-01-26
CN101027297A (zh) 2007-08-29
US20060040948A1 (en) 2006-02-23

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued

Effective date: 20130717